Amino acid derivatives containing chrysin were synthesized for evaluating their anticancer effects. Among them, compound -(7-((5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yl)oxy)heptanoyl)-L-isoleucine () displayed the most potent antiproliferative activity against MGC-803 cells with IC value of 20.0 μM. Preliminary mechanistic studies showed that compound could inhibit the colony formation and migration of MGC-803 cells. Flow cytometry analysis demonstrated that compound mediated cell apoptosis of MGC-803 cells and arrested cell cycle in G2/M-phase. Moreover, treatment in MGC-803 cells downregulated anti-apoptotic protein Bcl-2 and upregulated pro-apoptotic gene Bax in a concentration-dependent manner. Our studies suggest that compound may sever as an effective chemotherapeutic candidate. [Formula: see text].
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